Case Study 1

Title: Biphasic Release Tablet

The challenge: The client required a tablet which would release a proportion of an active compound immediately after swallowing and the remainder of the active released slowly over several hours.

The solution: The required drug release profile was achieved by incorporating a proportion of the drug in a tablet core (designed to retard the drug release) and coating the tablet core with a water soluble coating containing the remainder of the drug (providing an immediate release element.

Case Study 2

Title: Enhanced oral bioavailability for a poorly water soluble API - Tablet matrix

The challenge: The client presented an investigational drug which exhibited very poor water solubility, resulting in low and variable oral bioavailability (when administered in a capsule formulation). The project brief was to enhance the oral bioavailability of hte drug - preferably using a table formulation.

The solution: Two different table formulation strategies were considered:-

• Tablet 1 - Direct compression matrix
• Tablet 2 - Melt granulation-type matrixm, using a block copolomer as joint binding agent/solubilising agent.

The oral bioavailability for three presentations (Capsule formulation, Tablet 1 formulation and Tablet 2 formulation) was determined in human volunteers. The profiles obtained (mean values) are shown in the graph below.

As seen from the graph, the Tablet 2 formulation (containing the block compolymer) significantly improved the oral bioavailability of the API. Even the conventional table formulation (Tablet 1) exhibited a 50% increase in bioavailability.

Case Study 3

Title: Oral gel - for sublingual administration

The challenge: The client required a formulation for delivery of the API through buccal absorption, preferably as a water-based gel.

The solution: For efficient absorption through the buccal membrane it was necessary to adjust the pH to ensure that the API was in its non-ionised state - which consequently significantly reduced the water solubility of the API. Several solubility enhancing options were evaluated, including use of non-ionic surfactants and selection of suitable co-solvents.

A suitable gel formulation was successfully developed - which maintained the drug in its non-ionised form and retained it in solution- using a combination of co-solvents and an appropriate beta-cyclodextrin derivative.